enobosarm
Sign in to saveAlso known as ostarine, Ostarine, (2R)-3-(4-Cyanophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide, MK-2866
Enobosarm, also formerly known as ostarine and by the developmental code names GTx-024, MK-2866, and S-22, is a selective androgen receptor modulator (SARM) which is under development for the treatment of androgen receptor-positive breast cancer in women and for improvement of body composition (e.g., prevention of muscle loss) in people taking GLP-1 receptor agonists like semaglutide. It was also under development for a variety of other indications, including treatment of cachexia, Duchenne muscular dystrophy, muscle atrophy or sarcopenia, and stress urinary incontinence, but development for a
Research
110 papers- Muscle matters: the effects of medically induced weight loss on skeletal muscle.The lancet. Diabetes & endocrinology · 2024
- Cancer Cachexia: Its Mechanism and Clinical Significance.International journal of molecular sciences · 2021
- Activity and safety of enobosarm, a novel, oral, selective androgen receptor modulator, in androgen receptor-positive, oestrogen receptor-positive, and HER2-negative advanced breast cancer (Study G200802): a randomised, open-label, multicentre, multinational, parallel design, phase 2 trial.The Lancet. Oncology · 2024
- Study Design and Rationale for the Phase 3 Clinical Development Program of Enobosarm, a Selective Androgen Receptor Modulator, for the Prevention and Treatment of Muscle Wasting in Cancer Patients (POWER Trials).Current oncology reports · 2016
- Drug-Induced Liver Injury Secondary to Enobosarm: A Selective Androgen Receptor Modulator.Journal of medical cases · 2022
via PubMed
Wikidata facts
- Mass
- 389.099
Show 4 more facts
- Commons category
- Ostarine
- canonical SMILES
- CC(COC1=CC=C(C=C1)C#N)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O
- isomeric SMILES
- C[C@](COC1=CC=C(C=C1)C#N)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O
- chemical formula
- C₁₉H₁₄F₃N₃O₃
Sources (2)
via Wikidata · CC0
~39 min read
Article
23 sectionsContents
- Medical uses
- Side effects
- Overdose
- Interactions
- Pharmacology
- Pharmacodynamics
- Pharmacokinetics
- Absorption
- Distribution
- Metabolism
- Elimination
- Chemistry
- History
- Society and culture
- Names
- Non-medical use
- Doping in sport
- List of doping cases
- Research
- See also
- References
- Further reading
- External links
Enobosarm, also formerly known as ostarine and by the developmental code names GTx-024, MK-2866, and S-22, is a selective androgen receptor modulator (SARM) which is under development for the treatment of androgen receptor-positive breast cancer in women and for improvement of body composition (e.g., prevention of muscle loss) in people taking GLP-1 receptor agonists like semaglutide. It was also under development for a variety of other indications, including treatment of cachexia, Duchenne muscular dystrophy, muscle atrophy or sarcopenia, and stress urinary incontinence, but development for all other uses has been discontinued. Enobosarm was evaluated for the treatment of muscle wasting related to cancer in late-stage clinical trials, and the drug improved lean body mass in these trials, but it was not effective in improving muscle strength. As a result, enobosarm was not approved and development for this use was terminated. Enobosarm is taken by mouth.
Known possible side effects of enobosarm include headache, fatigue, anemia, nausea, diarrhea, back pain, adverse lipid changes like decreased high-density lipoprotein (HDL) cholesterol levels, changes in sex hormone concentrations like decreased testosterone levels, elevated liver enzymes, and liver toxicity, among others. The potential masculinizing effects of enobosarm, for instance in women, have largely not been evaluated and are unknown. The potential adverse effects and risks of high doses of enobosarm are also unknown. Enobosarm is a nonsteroidal SARM, acting as an agonist of the androgen receptor (AR), the biological target of androgens and anabolic steroids like testosterone and dihydrotestosterone (DHT). However, it shows dissociation of effect between tissues in preclinical studies, with agonistic and anabolic effects in muscle and bone, agonistic effects in breast, and partially agonistic or antagonistic effects in the prostate gland and seminal vesicles. The AR-mediated effects of enobosarm in many other androgen-sensitive tissues are unknown.